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| | Lorcaserin hydrochloride Basic information |
| Product Name: | Lorcaserin hydrochloride | | Synonyms: | (R)-1H-3-BENZAZEPINE,8-CHLORO-2,3,4,5-TETRAHYDRO-1-METHYL-,HYDROCHLORIDE;Lorcaserin hydrochloride;(R)-8-Chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride;(1R)-8-chloro-1-Methyl-2,3,4,5-tetrahydro-1H-3-benzazepine;lorcaserin hydrochloride (APD-356);R Lorcaserin hydrochloride;Green Card mianserin hydrochloride;(R)-1H-3-BENZAZEPINE | | CAS: | 846589-98-8 | | MF: | C11H15Cl2N | | MW: | 232.15 | | EINECS: | 1592732-453-0 | | Product Categories: | APIs;5-HT 2c receptor agonist;Inhibitors;1 | | Mol File: | 846589-98-8.mol |  |
| | Lorcaserin hydrochloride Chemical Properties |
| solubility | Soluble in DMSO > 10 mM | | form | Powder | | Stability: | Hygroscopic |
| | Lorcaserin hydrochloride Usage And Synthesis |
| Description | In June 2012, the US FDA approved lorcaserin for chronic weight management
in adult patients who are characterized as overweight or obese and
have at least one comorbid, weight-related condition.
Lorcaserin (also known as APD356) is the first 5-HT2C agonist
approved for chronic weight management since the withdrawal of the
5-HT2C agonist fenfluramine in 1997 due to rare cases of cardiac valvulopathy. The serotonin receptor 5-HT2C is found primarily in the hypothalamus
and regulates appetite and feeding behavior. Safety issues with
fenfluramine were associated with poor selectivity for 5-HT2C versus
5HT2A and 5HT2B. Ring constraint afforded by the benzazepine in
lorcaserin improved selectivity for 5HT2C by over 2 log units. | | Description | Lorcaserin (hydrochloride) (CRM) (Item No. 19247) is a certified reference material categorized as an anorectic. It also decreases oxycodone intake and has positive effects on self-administration and relapse vulnerability in the rat. Lorcaserin is regulated as a Schedule IV compound in the United States. This product is intended for research and forensic applications. | | Originator | Pharmaceuticals (United States) | | Uses | Lorcaserin hydrochloride, a novel antiobesity drug, is a selective serotonin 5-HT2C receptor agonist, approved by FDA in 2012. | | Definition | ChEBI: A hydrochloride obtained by reaction of lorcaserin with one equivalent of hydrochloric acid. Used as an anti-obesity drug. | | Brand name | Belviq | | Side effects | Lorcaserin hydrochloride (Belviq) is a serotonin 2C receptor agonist that causes weight loss by causing appetite suppression.It appears to have fewer adverse effects than orlistat,although long-term safety data are limited. The recommended dosage is 10mg twice daily. Lorcaserin should be discontinued if patients do not lose 5% of their body weight in 12 weeks. The efficacy of lorcaserin appears similar to that of orlistat (mean difference in weight loss between active and placebo-treated groups approximately 3-4 kg).Common side effects include nausea, headache,dizziness, nasopharyngitis, and fatigue. Lorcaserin may increasethe risk of symptomatic hypoglycemia in patients with type 2 diabetes on oral agents, necessitating a reduction in the dose of diabetes medications. Lorcaserin should not be used in individuals with creatinine clearance <30 mL/minute. It is contraindicated during pregnancy. In addition, lorcaserin should not be used with other serotonergic drugs (e.g., selective serotonin reuptake inhibitors,selective serotonin-norepinephrine reuptake inhibitors, bupropion[Wellbutrin], tricyclic antidepressants,and monamine oxidase inhibitors)because of the theoretical potential for serotonin syndrome.
https://www.accessdata.fda.gov
https://medlineplus.gov | | Drug interactions | Belviq (lorcaserin hydrochloride) may interact with antidepressants, including selective serotonin reuptake inhibitors (SSRIs), serotonin-norepinephrine reuptake inhibitors (SNRIs), monoamine oxidase inhibitors (MAOIs), triptans, bupropion, dextromethorphan, or St. John's Wort.
| | Precautions | The precautions of BELVIQ (lorcaserin hydrochloride) tablets:
Serotonin Syndrome or Neuroleptic Malignant Syndrome (NMS)- like Reactions: The safety of coadministration with other serotonergic or antidopaminergic agents has not been established.
Valvular heart disease: If signs or symptoms develop, consider BELVIQ discontinuation and evaluate the patient for possible valvulopathy.
Cognitive Impairment: This may cause disturbances in attention or memory. Caution with the use of hazardous machinery when starting BELVIQ treatment.
Psychiatric Disorders, including euphoria and dissociation: Do not exceed the recommended dose of 10 mg twice daily.
Monitor for depression or suicidal thoughts. Discontinue if symptoms develop.
Use of Antidiabetic Medications: Weight loss may cause hypoglycemia. Monitor blood glucose. BELVIQ has not been studied in patients taking insulin.
Priapism: Patients should seek emergency treatment if an erection lasts >4 hours. Use BELVIQ with caution in patients predisposed to priapism. |
| | Lorcaserin hydrochloride Preparation Products And Raw materials |
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